55510-47-9Relevant academic research and scientific papers
Development of Novel N-hydroxypyridone Derivatives as Potential Anti-Ischemic Stroke Agents
Hu, Linghao,Feng, Hongxuan,Zhang, Hongguang,Yu, Songda,Zhao, Qinyuan,Wang, Wei,Bao, Fengxia,Ding, Xun,Hu, Jiajing,Wang, Manjiong,Xu, Yixiang,Wu, Zengrui,Li, Xiaokang,Tang, Yun,Mao, Fei,Chen, Xiaoyan,Zhang, Haiyan,Li, Jian
supporting information, p. 1051 - 1067 (2020/03/10)
Our previous study had identified ciclopirox (CPX) as a promising lead compound for treatment of ischemic stroke. To find better neuroprotective agents, a series of N-hydroxypyridone derivatives based on CPX were designed, synthesized, and evaluated in this study. Among these derivatives, compound 11 exhibits significant neuroprotection against oxygen glucose deprivation and oxidative stress-induced injuries in neuronal cells. Moreover, compound 11 possesses good blood-brain barrier permeability and superior antioxidant capability. In addition, a complex of compound 11 with olamine-11·Ola possesses good water solubility, negligible hERG inhibition, and superior metabolic stability. The in vivo experiment demonstrates that 11·Ola significantly reduces brain infarction and alleviates neurological deficits in middle cerebral artery occlusion rats. Hence, compound 11·Ola is identified in our research as a prospective prototype in the innovation of stroke treatment.
Syntheses of α-pyrones using gold-catalyzed coupling reactions
Luo, Tuoping,Dai, Mingji,Zheng, Shao-Liang,Schreiber, Stuart L.
supporting information; experimental part, p. 2834 - 2836 (2011/07/07)
Sequential alkyne activation of terminal alkynes and propiolic acids by gold(I) catalysts yields compounds having α-pyrone skeletons. Novel cascade reactions involving propiolic acids are reported that give rise to α-pyrones with different substitution patterns.
Antifungal activity of 4-methyl-6-alkyl-2H-pyran-2-ones
Chattapadhyay, Tarun Kumar,Dureja, Prem
, p. 2129 - 2133 (2007/10/03)
A number of 4-methyl-6-alkyl-α-pyrones were synthesized and characterized on the basis of 1H NMR and mass spectroscopy. These compounds were tested in vitro against pathogenic fungi, namely, Sclerotium rolfsii Saccardo, Rhizoctonia bataticola (Taub.) Butler, Pythium aphanidermatum (Edson) Fitz., Macrophomina phaseolina (Tassi), Pythium debaryanum (Hesse), and Rhizoctonia solani Nees. Lower homologues were less effective, whereas compounds such as 4-methyl-6-butyl-α-pyrone, 4-methyl-6-pentyl-α-pyrone, 4-methyl-6-hexyl-α-pyrone, and 4-methyl-6-heptyl-α-pyrone were found effective against all of the test fungi. They inhibited mycelial growth by approximately 50% (ED50) at 15-50 μg/mL. 4-Methyl-6-hexyl-α- pyrone, which was found most effective, was tested against S. rolfsii in a greenhouse at 1, 5, and 10% concentrations. The 10% aqueous emulsion of 4-methyl-6-hexyl-α-pyrone suppressed disease development in tomato by 90-93% as compared with the untreated infested soil in the greenhouse after 35 days of treatment.
Regio- and stereoselective preparation of γ-alkylidenebutenolides or α-pyrones using a Stille reaction and palladium-catalysed oxacyclisation sequence
Rousset, Séverine,Abarbri, Mohamed,Thibonnet, Jér?me,Parrain, Jean-Luc,Duchêne, Alain
, p. 7633 - 7636 (2007/10/03)
Synthesis of butenolides or α-pyrones from substituted tributylstannyl acetylides is highly dependant on the nature of the acetylide.
Fungicide comprising 4-methyl-6-pentyl-2H-pyran-2-one
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, (2008/06/13)
The invention provides a fungicidal composition comprising the compound 4-methyl-6-pentyl-2H-pyran-2-one and one or more suitable carriers, adjuvants and/or diluents. Also provided is a method of preventing or at least inhibiting the growth of fungi which comprises the step of applying the compound of the fungi or their locus. Further provided is a process for preparing the compounds.
